Additional Hetero Ring Patents (Class 514/202)
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Patent number: 5541177Abstract: A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4)alkylamino-;Y represents CH or N;Y" represents (a) CR.sup.y' R.sup.z' with R.sup.y' and R.sup.z' hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH.Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: June 6, 1995Date of Patent: July 30, 1996Assignee: Merck & Co., Inc.Inventors: Lovji D. Cama, James V. Heck
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Patent number: 5541176Abstract: Cephalosporin compounds of the formula I ##STR1## are disclosed. The compounds are useful against MRSA/MRCNS. Compositions and methods of use are also included.Type: GrantFiled: May 26, 1995Date of Patent: July 30, 1996Assignee: Merck & Co., Inc.Inventors: Lovji D. Cama, Mary F. Sasor, Milton L. Hammond
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Patent number: 5534507Abstract: A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-;Y represents CH or N;Y" represents (a) CR.sup.y 'R.sup.z ' with R.sup.y ' and R.sup.z ' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH.Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical editions and methods of use are also included.Type: GrantFiled: June 6, 1995Date of Patent: July 9, 1996Assignee: Merck & Co., Inc.Inventors: Lovji D. Cama, James V. Heck
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Patent number: 5523400Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sup.1 is an acyl group derived from a carboxylic acid, hydrogen, or an amino protecting group;R.sup.2 is hydrogen, hydroxy, lower alkyl-Q.sub.p -, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl-Q.sub.p -, aryl-Q.sub.p -, aryloxy, aralkoxy or a heterocyclic ring, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, oxo, cycloalkyl, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, --CONR.sup.4 R.sup.5, --N(R.sup.5)COOR.sup.9, R.sup.5 CO--, R.sup.5 OCO-- or R.sup.5 COO-- where R.sup.4 is hydrogen, lower alkyl, or cycloalkyl; R.sup.5 is hydrogen or lower alkyl; R.sup.9 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;Q is --CO-- or --SO.sub.Type: GrantFiled: March 21, 1994Date of Patent: June 4, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Chung-Chen Wei, Peter Angehrn
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Patent number: 5514561Abstract: Chromogenic and fluorogenic substrates for .beta.-lactamase, methods for synthesis thereof and methods for detecting .beta.-lactamase in a sample are provided. The substrates are substantially colorless or substantially nonfluorescent .beta.-lactam compounds which include an electronegative leaving group. The leaving group comprises a carbamate, carbonate, thiocarbamate or thiocarbonate linkage and a fluorescent moiety or a moiety capable of producing a visually detectable colored product. Upon cleavage of the lactam ring by .beta.-lactamase, the leaving group is liberated and fluorescence or a colored product is produced.Type: GrantFiled: April 14, 1994Date of Patent: May 7, 1996Assignee: Becton, Dickinson and CompanyInventors: J. Michael Quante, Randal A. Hoke, Patrick D. Mize, Daniel L. Woodard, O. Elmo Millner, deceased
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Patent number: 5498777Abstract: Cephalosporin compounds of the formula I ##STR1## are disclosed. The compounds are useful against MRSA/MRCNS. Compositions and methods of use are also included.Type: GrantFiled: July 20, 1994Date of Patent: March 12, 1996Assignee: Merck & Co., Inc.Inventors: Lovji D. Cama, Mary F. Sasor, Milton L. Hammond
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Patent number: 5480879Abstract: The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are linked to a .beta.-lactam antibiotic, to their salts, to processes for their preparation and to antibacterial agents containing these derivatives.Type: GrantFiled: October 1, 1993Date of Patent: January 2, 1996Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Wilfried Schrock, Dieter Habich, Andreas Krebs, Thomas Schenke, Thomas Philipps, Klaus Grohe, Rainer Endermann, Klaus-Dieter Bremm, Karl-Georg Metzger
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Patent number: 5461043Abstract: Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(metho xymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.Type: GrantFiled: September 3, 1992Date of Patent: October 24, 1995Assignee: Hoechst AktiengesellschaftInventors: Gerd Fischer, Elisabeth Defossa, Uwe Gerlach, Rolf Horlein, Norbert Krass, Rudolf Lattrell, Ulrich Stache, Theodor Wollmann, Dieter Isert
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Patent number: 5455238Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## in the form of an internal salt or a non-toxic, pharmaceutically acceptable acid addition salt wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are individually defined in the specification, R.sub.4 is --OH or alkoxy of 1 to 8 carbon atoms, A and A' are individually selected from the group consisting of hydrogen, an equivalent of an alkali metal or alkaline earth metal, magnesium, ammonium and an organic amine, or one or two of --COOA or --COOA' ARE --CO.sub.2 --, the wavy line means --CH.sub.2 R.sub.6 can be in the E or Z position, R.sub.6 in the quaternary ammonium form is selected from the group consisting of ##STR2## X is defined as in the specification with the proviso that when R.sub.3 is --OH or alkoxy of 1 to 8 carbon atoms, at least one R.sub.1, R.sub.2 and R.sub.5 is other than hydrogen having antibacterial properties.Type: GrantFiled: December 11, 1992Date of Patent: October 3, 1995Assignee: Roussel UclafInventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert
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Patent number: 5455239Abstract: A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-;Y represents CH or N;Y" represents (a) CR.sup.y' R.sup.z' with R.sup.y' and R.sup.z' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH.Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: August 5, 1993Date of Patent: October 3, 1995Assignee: Merck & Co. Inc.Inventors: Lovji D. Cama, James V. Heck
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Patent number: 5446037Abstract: This invention relates to 2-[(substituted)methylene]cephalosporin sulfones and in particular 2-[(heteroaryl substituted)methylene]cephalosporin sulfones which are effective elastase inhibitors as well as effective thrombin inhibitors and therefore are useful as anti-inflammatory, anti-degenerative and anti-thrombin agents.Type: GrantFiled: December 13, 1993Date of Patent: August 29, 1995Assignee: Synphar Laboratories, Inc.Inventors: Samarendra Maiti, Charles Fiakpui, A. V. N. Reddy, David Czajkowski, Paul Spevak, Harninder Atwal, Ronald G. Micetich
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Patent number: 5439904Abstract: 2-spiro (2'-spirocycloalkyl) cyclopropyl cephalosporin sulfone compounds, methods of treating patients for elastase inhibition, and processes for preparing such compounds.Type: GrantFiled: December 7, 1993Date of Patent: August 8, 1995Assignee: Synphar Laboratories, Inc.Inventors: Samarendra N. Maiti, Charles Y. Fiakpui, Andhe V. N. Reddy, David P. Czajkowski, Ronald G. Micetich
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Patent number: 5438052Abstract: Cephalosporin derivatives have the formula ##STR1## wherein Z.sup.1, Z.sup.2, X, Y, P, Q, m, n and p are as defined in the following text. Also described are the readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, and hydrates of compounds of formula I, their esters and salts. Processes are provided for manufacture and pharmaceutical preparations which contain these compounds. Intermediates from the manufacture of these compounds are described, as is the use of the compounds in the control of illnesses and for the manufacture of the aforementioned preparations.Type: GrantFiled: November 20, 1992Date of Patent: August 1, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Peter Angehrn, Andre Furlenmeier, Paul Hebeisen, Werner Hofheinz, Helmut Link
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Patent number: 5416080Abstract: A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein the substituents are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.Type: GrantFiled: June 21, 1993Date of Patent: May 16, 1995Assignee: Roussel-UCLAFInventors: Jozsef Aszodi, Jean-Francois Chantot, Solange Gouin D'Ambrieres
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Patent number: 5409917Abstract: A method and composition for topically treating acne and acneiform dermal disorders includes applying an amount of a cephalosporin antibiotic effective to treat the acne and acneiform dermal disorders. The antibiotic is blended with a carrier suitable for topical application to dermal tissues. The carrier is selected from the group consisting of an aqueous liquid, an alcohol base, a water soluble gel, a lotion, an ointment, a nonaqueous liquid base, a mineral oil base, a blend of mineral oil and petrolatum, liposomes, a time-release patch, and a liquid-absorbed wipe. The cephalosporin can also be combined with benzoyl peroxide in a gel carrier.Type: GrantFiled: September 24, 1993Date of Patent: April 25, 1995Assignees: Marvin S. Towsend, Leonard BloomInventors: Howard N. Robinson, Neil F. Martin
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Patent number: 5409918Abstract: Crystalline cephem acid addition salts of the general formula II ##STR1## pharmaceutical preparations effective against bacterial infections which contain such cephem derivatives, processes for the preparation of the cephem derivatives and the pharmaceutical preparations, and the use of the cephem derivatives for combating bacterial infections.Type: GrantFiled: August 21, 1992Date of Patent: April 25, 1995Assignee: Hoechst AktiengesellschaftInventors: Friedhelm Adam, Walter Durckheimer, Burkhard Mencke, Dieter Isert
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Patent number: 5409919Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sup..sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.Type: GrantFiled: April 2, 1993Date of Patent: April 25, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Masahiro Kondo, Masahiko Fujino
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Patent number: 5401842Abstract: The present invention provides physical admixtures of a new crystalline dihydrochloride dihydrate salt of the cephalosporin antibiotic, cefepime with a pharmaceutically acceptable non-toxic organic or inorganic base. In particular, this invention provides physical admixtures having a temperature and moisture stable crystalline dihydrochloride dihydrate form of cefepime having a specific X-ray powder diffraction pattern as described herein.Type: GrantFiled: February 18, 1994Date of Patent: March 28, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Munir N. Nassar, Murray A. Kaplan
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Patent number: 5397779Abstract: A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein R.sub.1, Rc, Rb, A and A' are defined as in the following specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.Type: GrantFiled: December 7, 1992Date of Patent: March 14, 1995Assignee: Roussel-UclafInventors: Jozsef Aszodi, Jean-Francois Chantot, Solange G. D'Ambrieres
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Patent number: 5389627Abstract: The present invention relates to novel cephem compounds having the formula: ##STR1## wherein, Q is a carbon or nitrogen atom; X is an oxygen atom, or a nitroalkyl or cyanoimine group, with the proviso that X cannot be an oxygen atom when Q is a carbon atom; R.sub.1 is a hydrogen atom, or a lower alkyl group, or a lower alkyl group which may be substituted by fluoro, or by a carboxylic group or an inorganic cation salt thereof; and R.sub.2 and R.sub.3 independently are a hydrogen atom or a lower alkyl group; or pharmaceutically acceptable salts thereof.The compounds of the present invention have potent antibacterial activities against gram-negative bacteria, especially Pseudomonas, and a longer half-life than conventional cephem compounds.Type: GrantFiled: November 3, 1993Date of Patent: February 14, 1995Assignee: Cheil Foods & ChemicalsInventors: Choong S. Kim, Yang S. Ahn, Kang Y. Jung, Nam H. Lee, Rok L. Yun, Seong Y. Park, Yeo H. Yoon, Keon H. Lee, Chun S. Lyu, Kwang H. Lee
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Patent number: 5389626Abstract: Compounds of formula (I): ##STR1## in which: R.sup.1 is hydrogen or acyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkoxy; and Ar is phenyl or substituted phenyl and pharmaceutically acceptable salts and esters thereof have valuable antibiotic activity, including against Methicillin-resistant strains of Staphylococcus. The invention also provides a process for preparing the compounds and methods and compositions using them.Type: GrantFiled: May 5, 1992Date of Patent: February 14, 1995Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Kazuo Koyama, Shigeo Amemiya, Masayuki Iwata
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Patent number: 5389625Abstract: Cephalosporin compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen atom or lower alkyl, and R.sup.2 is 1-alkanoyloxyalkyl or 1-alkoxycarbonyloxyalkyl, their pharmaceutically acceptable salts, methods for producing them, and pharmaceutical use thereof.The cephalosporin compounds and their salts are superior in absorption from digestive tract, and upon absorption from the digestive tract, show a wide range of antimicrobial activities in the body as hydrolysis products, and in addition, they have 10-400 times greater sweetness than sucrose. Thus, said compounds are useful as agents to be administered orally for the prophylaxis and treatment of bacterial infectious diseases.Type: GrantFiled: June 8, 1992Date of Patent: February 14, 1995Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroyuki Muro, Masayasu Kasai, Satoru Hatano, Ken-ichi Nishimura, Susumu Nishizawa, Nobuharu Kakeya
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Patent number: 5373000Abstract: A cephalosporin derivative represented by the formula: ##STR1## wherein R.sub.1 represents a lower alkyl group, and A is selected from: a group of the following formula: ##STR2## where R.sub.2 and R.sub.3 are the same or different lower alkyl group, R.sub.4 represents a substituted lower alkyl or amino group;a group which may be substituted and which is represented by the following formula: ##STR3## where R.sub.5 represents a lower alkyl group; or a group of the following formula: ##STR4## where R.sub.5 is as defined above, R.sub.6 represents a hydroxyl lower alkyl or carboxyl group, or its pharmacologically acceptable salt, and a process for preparing the same, as well as an antibacterial agent containing the same.Type: GrantFiled: April 1, 1992Date of Patent: December 13, 1994Assignee: Eisai Co., Ltd.Inventors: Yoshimasa Machida, Takashi Kamiya, Shigeto Negi, Toshihiko Naito, Yuuki Komatu, Seiichiro Nomoto, Isao Sugiyama, Hiroshi Yamauchi
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Patent number: 5373001Abstract: A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of a R, S mixture wherein the various substituents are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.Type: GrantFiled: July 22, 1993Date of Patent: December 13, 1994Assignee: Roussel UclafInventors: Jozsef Aszodi, Jean-Francois Chantot, Solange G. D'Ambrieres
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Patent number: 5366970Abstract: The invention relates to a compound of the formula: ##STR1## of antimicrobial activity.Type: GrantFiled: September 2, 1992Date of Patent: November 22, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazuo Sakane, Kohji Kawabata, Yoshiko Inamoto
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Patent number: 5364848Abstract: New substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.Type: GrantFiled: May 1, 1992Date of Patent: November 15, 1994Assignee: Merck & Co., Inc.Inventors: James B. Doherty, Raymond A. Firestone, Paul E. Finke, William K. Hagmann, Shrenik K. Shah, Kevan R. Thompson
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Patent number: 5362722Abstract: The present invention provides compounds of the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl;A and A' are independently hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, amino, a 5-6 membered organic heterocycle containing 1, 2, or 3 hetero atoms selected from nitrogen or sulfur, C.sub.1 -C.sub.6 alkoxy, or phenyl; or A and A' taken together form a group of the formulae ##STR2## wherein X is hydrogen, halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, amino, nitro, or carboxy; and Y is nitrogen or carbon; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions and methods of treatment using the above compounds.Type: GrantFiled: December 23, 1992Date of Patent: November 8, 1994Assignee: Eli Lilly and CompanyInventor: Robert J. Ternansky
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Patent number: 5350753Abstract: Pharmaceutical combination preparations containing cefotaxime and at least one xanthine derivative are suitable for the treatment of bacterial infectious diseases and for the treatment of septic shock.Type: GrantFiled: June 18, 1991Date of Patent: September 27, 1994Assignee: Hoechst AktiengesellschaftInventors: Norbert Klesel, Michael Limbert, Elmar Schrinner
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Patent number: 5348951Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described,--CH.sub.2 --Y--Q (I)wherein Y is a bond or a linking group --NR.sup.4 --Y'--, --O--Y'--, --S--Y'-- wherein R.sup.4 is hydrogen, various optionally substituted alkyl groups, alkenyl, alkanoyl or alkanesulphonyl, and Y' is a bond or various optionally substituted alkylene groups; and Q is a benzene ring (optionally fused to a further benzene ring so forming a naphthyl group or optionally fused to a 5 or 6 membered heterocyclic aromatic group containing 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur), said benzene ring being substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or Q is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.Type: GrantFiled: September 5, 1991Date of Patent: September 20, 1994Assignee: ICI PharmaInventor: Frederic H. Jung
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Patent number: 5348952Abstract: Cephalosporins of the formula (I): ##STR1## wherein m is one or two; n is zero, one or two; A and B are organic residues; and R.sub.1 and R.sub.2 are halogen or hydrogen atoms or organic groups are endowed with elastase inhibitory activity. Two processes for their preparation starting from the corresponding 4-acyl cephem are also provided.Type: GrantFiled: June 12, 1992Date of Patent: September 20, 1994Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Pierluigi Bissolino, Marco Alpegiani, Ettore Perrone, Piergiuseppe Orezzi, Giuseppe Cassinelli, Giovanni Franceschi
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Patent number: 5336673Abstract: The present invention relates to novel cephalosporins of the formula (I); ##STR1## wherein, R.sub.1 represents a C.sub.1 .about.C.sub.4 alkyl group or ##STR2## wherein, R.sub.2 and R.sub.3, independently, represent hydrogen or a C.sub.1 .about.C.sub.3 alkyl group and R.sub.4 represents hydrogen or a C.sub.1 .about.C.sub.4 alkyl group;R.sub.1a represents hydrogen or an amino-protecting group;Q represents CH or N; andthe formula ##STR3## represents a saturated or unsaturated heterocyclic group which contains 1 to 4 nitrogen atoms of which one is substituted with an amino group to form quaternary ammonium, and oxygen or sulfur, or a fused heterocyclic group thereof formed together with a substituted or unsubstituted benzene or an optional heterocyclic group, or a pharmaceutically acceptable salt thereof, to processes for preparing the same and to a pharmaceutical composition containing the same as an active ingredient.Type: GrantFiled: February 26, 1992Date of Patent: August 9, 1994Assignee: Dae Woong Pharmaceutical Co., Ltd.Inventors: Chi J. Moon, Sae C. Park, Myoung G. Kim, Sea H. Oh, Seong S. Yim, Nam J. Park, Young K. Choi, Moo J. Sung
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Patent number: 5324721Abstract: The invention relates to new 3-substituted cephalosporins, a process for their preparation and their use as medicaments, in particular as medicaments having antibacterial activitity.Type: GrantFiled: September 19, 1991Date of Patent: June 28, 1994Assignee: Bayer AktiengesellschaftInventors: Stephan Schneider, Rainer Endermann, Karl-Georg Metzger, Klaus-Dieter Bremm
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Patent number: 5318781Abstract: The oral absorption of antibiotics given of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of Laureth-12 together with a second component salts of capric acid and caprylic acids. The antibiotic containing two component enhancer system includes Miglyol-812 for optimum absorption.Type: GrantFiled: April 6, 1993Date of Patent: June 7, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Navnit Shah, Joel Unowsky
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Patent number: 5312813Abstract: A method of killing microorganisms which form a biofilm on a tissue or implant surfaces in a patient, and which are refractory to a biocide at a dose which is effective to kill the microorganism in planktonic form. The effect of the biocide is potentiated, to an effective killing level, by applying an electric field across the surface containing the biofilm.Type: GrantFiled: July 22, 1992Date of Patent: May 17, 1994Assignee: University Technologies InternationalInventors: John W. F. Costerton, Antoine E. Khoury, Frank Johnson
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Patent number: 5306717Abstract: Cephalosporin derivatives of the general formula ##STR1## pharmaceutical preparations which are active against bacterial infections and contain such cephem derivatives, processes for the preparation of the cephem derivatives and the pharmaceutical preparations and the use of the cephem derivatives for combating bacterial infections.Type: GrantFiled: July 24, 1992Date of Patent: April 26, 1994Assignee: Hoechst AktiengesellschaftInventors: Friedhelm Adam, Walter Durckheimer, Gerd Fischer, Burkhard Mencke, Gerhard Seibert, Dieter Isert, Norbert Klesel
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Patent number: 5302712Abstract: The invention relates to compounds, useful as intermediates in the preparation of products of antimicrobial activity, of the formula: ##STR1## wherein R.sup.3 is hydrogen, lower alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, amino(lower)alkyl, protected amino (lower) alkyl, carbamoyl)lower)alkyl, N,N-di(lower) alkylcarbamoyl(lower)alkyl or an amino protective group, andR.sup.4 is hydrogen, lower alkyl, carboxy, protected carboxy, amino, protected amino or carbamoyl,or a salt thereof.Type: GrantFiled: February 23, 1993Date of Patent: April 12, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazuo Sakane, Kohji Kawabata, Yoshiko Inamoto
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Patent number: 5276024Abstract: The invention relates to new 3-substituted cephalosporins, to a process for their preparation and to their use as medicaments, in particular as medicaments having antibacterial activity.The invention relates to compounds of the general formula (I) ##STR1## in which X, Y, R.sup.1 and R.sup.2 have the meaning indicated in the description.Type: GrantFiled: November 21, 1991Date of Patent: January 4, 1994Assignee: Bayer AktiengesellschaftInventors: Stephan Schneider, Rainer Endermann, Karl G. Metzger, Klaus-Dieter Bremm
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Patent number: 5264429Abstract: Derivatives of 2-spirocyclopropyl cephalosporin sulfone of the structural formula I ##STR1## are provided which are useful as potent elastase inhibitors.Type: GrantFiled: August 20, 1991Date of Patent: November 23, 1993Assignee: SynPhar Laboratories, Inc.Inventors: Samarendra N. Maiti, David Czajkowski, Paul Spevak, Kazuo Adachi, Ronald G. Micetich
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Patent number: 5264430Abstract: Derivatives of 2-spirocyclopropyl cephalosporin sulfone of the structural formula I ##STR1## are provided which are useful as potent elastase inhibitors.Type: GrantFiled: April 8, 1991Date of Patent: November 23, 1993Assignee: SynPhar Laboratories, Inc.Inventors: Samarendra N. Maiti, David Czajkowski, Paul Spevak, Kazuo Adachi, Ronald G. Micetich
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Patent number: 5262410Abstract: Cephalosporin compounds having a 3-position substituent of the formula (I) are described:--CH.sub.2 --S--Q--(Y).sub.n --Pwherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring substituted by groups R.sup.1 and R.sup.2 which are ortho with respect to one another, wherein R.sup.1 is hydroxy or an in vivo hydrolysable ester thereof and R.sup.2 is hydroxy, an in vivo hydrolysable ester thereof, carboxy, sulpho, hydroxymethyl, methanesulphonamido or ureido; or P is a group of the formula (II) or (III): ##STR1## wherein M is oxygen or a group NR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl; said ring P being further optionally substituted; and --(Y).sub.n -- is a bond or various linking groups or --(Y)--.sub.n may be such so that rings Q and P are fused.The use of such compounds as antibacterial agents is described as are processes for their preparation and intermediates therefor.Type: GrantFiled: August 5, 1991Date of Patent: November 16, 1993Assignee: ICI PharmaInventors: Frederic H. Jung, Annie A. Olivier
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Patent number: 5258377Abstract: Derivatives of 2-spirocyclopropyl 4-acylcephem sulfones of the formula (I) ##STR1## are provided which are useful as potent elastase inhibitors and hence are useful in the prevention, control and treatment of inflammatory conditions, especially arthritis and emphysema.Type: GrantFiled: April 8, 1991Date of Patent: November 2, 1993Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Samarendra N. Maiti, Narender A. V. Reddy, David Czajkowski, Paul Spevak, Charles Fiakpui, Ronald G. Micetich
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Patent number: 5254545Abstract: A preparation containing a cephalosporin medicament is disclosed. The preparation comprises a cephalosporin derivative represented by the following formula: ##STR1## namely, 7.beta.-{2-(5-amino-1,2,4-thiadiazol-3-yl)-(Z)-2-fluoromethoxyiminoacetami do}-3-{(E)-3-(carbamoylmethylethylmethylammonio) -1-propen-1-yl}-3-cephem-4-carboxylate or a pharmaceutically acceptable salt thereof salt, lactose, citric acid or a sodium salt thereof, and arginine or a hydrochloride thereof; or the cephalosporin derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof, lactose, citric acid or a sodium salt thereof, and sodium chloride.Type: GrantFiled: September 28, 1990Date of Patent: October 19, 1993Assignee: Eisai Co., Ltd.Inventors: Yasuo Ishibashi, Isamu Hasegawa, Masanori Kayano, Ryoichi Machida, Masahiro Kawahara, Sumio Watanabe
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Patent number: 5246926Abstract: .beta.-Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: ##STR1## wherein R.sup.1 is hydrogen, methoxy or formamido;R.sup.2 is an acyl group, in particular that of an antibacterially active cephalosporin;CO.sub.2 R.sup.6 is a carboxy group or a carboxylate anion;R.sup.3 is a Y-lactone ring optionally containing an endocyclic double bond, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; and X is S, SO, SO.sub.2, O or CH.sub.2.Type: GrantFiled: March 28, 1990Date of Patent: September 21, 1993Assignee: Beecham Group p.l.c.Inventors: John H. Bateson, George Burton, Stephen C. M. Fell
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Patent number: 5244890Abstract: Cephem compounds having the following formula are disclosed: ##STR1## R.sup.1 =amino or protected amino R.sup.2 =an organic group ##STR2## R.sup.6 =lower alkyl R.sup.7, R.sup.8 .dbd.OH or protected OHY.dbd.N or CHThe compounds are useful as antimicrobial agents.Type: GrantFiled: May 20, 1992Date of Patent: September 14, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hideaki Yamanaka, Yoshiki Yoshida, Jiro Goto, Takeshi Terasawa, Shinya Okuda, Kazuo Sakane
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Patent number: 5244891Abstract: Crystalline sulfuric, di-nitric, mono-hydrochloric, di-hydrochloric, and di- and sesqui-orthosphosphoric acid addition salts of 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(Z)-methoxyiminoacetamido]-3-[(1- methyl-1-pyrrolidinio)methyl]-3-cephem-4-carboxylate are stable even at elevated temperatures. The crystalline sulfuric acid addition salt is made by forming an admixture of (a) at least one molar equivalent of sulfuric acid with (b) zwitterion in an amount so as to be present in the admixture at a concentration of greater than 25 milligrams/ml, causing crystallization, separating the crystals, washing and drying. The crystalline monohydrochloride, dihydrochloride, and orthophosphate salts are prepared by dissolving the zwitterion in the appropriate amount of acid, causing crystallization by adding acetone and isolating the crystals. Physical admixtures of the salts with certain bases in proportions to give a pH ranging from about 3.Type: GrantFiled: May 22, 1992Date of Patent: September 14, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Murray A. Kaplan, Thomas W. Hudyma, Robert A. Lipper, Kun M. Shih, Susan D. Boettger
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Antibiotic C-7 catechol-substituted cephalosporin compounds, compositions, and method of use thereof
Patent number: 5234920Abstract: The present invention relates to new cephalosporins of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or carboxy, with the proviso that both cannot be the same;R.sup.3 is hydrogen or acetyl; andR.sup.4 is a radical selected from the group consisting of ##STR2## in which n is 1 or 2, R.sup.5 is hydrogen or acetyl, and R.sup.6 is hydrogen, a lower C.sub.1-3 alkyl, or a radical selected from the group consisting of ##STR3## in which n and R.sup.5 are as defined above. In another aspect, this invention relates to processes for the preparation of the compounds of Formula I, to pharmaceutical compositions containing at least one compound of Formula I, and to intermediates in their preparation.Type: GrantFiled: January 6, 1992Date of Patent: August 10, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Takaaki Okita, Hajime Kamachi, Shinji Masuyoshi, Kiyoto Imae -
Patent number: 5232918Abstract: Cephalosporin derivatives having a 3-position substituent of formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atom;R.sup.2 is hydroxy or an in vivo hydrolysable ester thereof;R.sup.3 is ortho to R.sup.2 and is hydroxy or an in vivo hydrolysable ester thereof; and R.sup.Type: GrantFiled: February 11, 1991Date of Patent: August 3, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Jean C. Arnould, Dominique Boucherot, David H. Davies, Frederick H. Jung, Colin J. Strawson
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Patent number: 5223496Abstract: Cephalosporin compounds of Formulas II ##STR1## where R is hydrogen or a pharmaceutical cation, in which case R.sub.1 is not present, orR is hydrogen or a chemical bond when R.sub.1 is an acid addition salt anion, and R.sub.2 is (a) hydrogen, (b) a duplicate of the formula I compound to form a dimer, (c) an aminocarbonylmethyl, or (d) an --SR.sub.3 group where R.sub.3 is alkyl, cyclohexyl, phenyl, chloro-substituted phenyl, nitro-substituted phenyl, benzyl or furfuryl, have been found to be valuable as antibiotics for treating warm-blooded animals to combat pathogenic bacterial infections which cause diseases such as the commonly known "shipping fever".Type: GrantFiled: April 23, 1992Date of Patent: June 29, 1993Assignee: The Upjohn CompanyInventors: Alexander R. Cazers, K. Thomas Koshy, Prem S. Jaglan, Robert J. Yancey, Jr., Terry J. Gilbertson, Thomas S. Arnold, David B. Johnson, Catherine L. Gatchell
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Patent number: 5219848Abstract: Cephalosporin antibiotics having a 3-position substituent of the formula: ##STR1## are described, wherein X is --CO--, --SO.sub.2 -- or --COCH.sub.2 --; Y is --CO--, --SO.sub.2 -- or --CH.sub.2 --; Q is a benzene, pyridine or naphthalene ring, R.sup.1 and R.sup.2 are ortho with respect to each other and are independently hydroxy or of the formula O--M wherein M is a moiety and the O--M bond is cleavable in vivo and ring Q may be further substituted by a variety of atoms and groups. Processes for their preparation and use are described.Type: GrantFiled: August 10, 1990Date of Patent: June 15, 1993Assignees: ICI Pharma, Imperial Chemical Industries PLCInventors: Laurent F. A. Hennequin, David M. Hollinshead
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Patent number: RE34865Abstract: Cephemcarboxylic acid esters of the general formula ##STR1## pharmaceutical preparations which are active against bacterial infections, which contain such cephem derivatives, a process for the preparation of the cephem derivatives and the pharmaceutical preparations, and also the use of the cephem derivatives for combating bacterial infections.Type: GrantFiled: November 19, 1992Date of Patent: February 21, 1995Assignee: Hoechst AktiengesellschaftInventors: Friedhelm Adam, Jurgen Blumbach, Walter Durckheimer, Gerd Fischer, Burghard Mencke, Dieter Isert, Gerhard Seibert